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Hypertensive Emergency - IV Agents

Background

Hypertensive emergency - definition: Severe hypertension that is associated with acute end-organ damage. Examples include malignant hypertension, with or without hypertensive encephalopathy, subarachnoid or intracerebral hemorrhage, acute pulmonary edema, aortic dissection, and rebound after withdrawal of antihypertensive medications. Immediate but careful reduction in blood pressure is indicated in these settings. However, an excessive hypotensive response is potentially dangerous, possibly leading to ischemic complications such as stroke, myocardial infarction or blindness in some cases. Thus, in patients who are severely hypertensive but asymptomatic, slower reductions in blood pressure should be provided with oral agents. Source: UpToDate ®
Enalaprilat - Vasotec ® Esmolol - Brevibloc ®
Fenoldopam mesyl. -Corlopam ® Hydralazine - APRESOLINE ®
Labetalol - Trandate ® Nicardipine - Cardene ®
Nitroglycerin Sodium nitroprusside - Nipride ®
Please see package insert for additional information and possible updates. The authors make no claims of the accuracy of the information contained herein; and these suggested doses are not a substitute for clinical judgment. Neither GlobalRPh Inc. nor any other party involved in the preparation of this program shall be liable for any special, consequential, or exemplary damages resulting in whole or part from any user's use of or reliance upon this material. PLEASE READ THE DISCLAIMER CAREFULLY BEFORE ACCESSING OR USING THIS SITE. BY ACCESSING OR USING THIS SITE, YOU AGREE TO BE BOUND BY THE TERMS AND CONDITIONS SET FORTH IN THE DISCLAIMER.    [  Read the disclaimer    |   <<Back     ]

Enalaprilat - Vasotec ®  top of page

ACE-inhibitor with a rapid onset of action and long duration of action.
Dosing (Adult): Initial dose 1.25 mg IV push (over 2 to 5 minutes) q6h. May increase up to 5 mg q6h. Reduce dose in azotemic patients. Contraindicated in renal artery stenosis. Onset/duration: Within 15 to 30 minutes/12-24 hr. Note: peak effect may not be seen for four hours.

Esmolol - Brevibloc ®  top of page

Beta-1 selective blocker. Rapidly metabolized by blood esterases (short half-life ~ 9 minutes) and total duration of action ~ 30 minutes. Its effects begin almost immediately.
Dosing (Adult): 500 mcg/kg IV bolus over 1 minute, and start infusion at 50 - 100 mcg/kg/min => repeat bolus dose of 500 mcg/kg if no effect within 5 minutes and increase dose by 50 mcg/kg/min. Repeat cycle every 5 minutes until maximum infusion dose of 300 mcg/kg/min.

Contraindicated in cocaine toxicity (if used alone) and LVF and COPD/asthma and high-grade heart block. Causes phlebothrombophlebitis - use large vein's. Causes local necrosis if extravasation occurs.

Onset/duration
:1-5 min/15-30 min.

Fenoldopam mesylate - Corlopam ®  top of page

Fenoldopam is a rapid-acting vasodilator. It is an agonist for D1-like dopamine receptors and binds with moderate affinity to alpha2-adrenoceptors. Fenoldopam: effective as nitroprusside, however, it has the advantages of increasing renal blood flow (6 times as potent as dopamine in producing renal vasodilitation) and sodium excretion, of not being associated with the accumulation of toxic metabolites, and not requiring shielding from light. Fenoldopam can be safely used in all hypertensive emergencies, and may be particularly beneficial in patients with renal insufficiency.

Dosing (Adult): After a starting dose of 0.1 to 0.3 mcg/kg/minute, the dose is titrated at 15 minute intervals, depending on the BP response. May be increased in increments of 0.05 to 0.1 mcg/kg/minute every 15 minutes until target blood pressure is reached. Maximal infusion rate reported in clinical studies: 1.6 mcg/kg/minute. Onset/duration: 5-10 minutes/~ 1 hour.

Supplied: Injection (soln): 10 mg/mLl(1 ml, 2 ml)

Hydralazine - APRESOLINE ®  top of page

Direct arteriolar vasodilator with little or no effect on the venous circulation. Precautions are needed in patients with underlying coronary disease or an aortic dissection. Beta-blocker should be given concurrently to minimize reflex sympathetic stimulation. The hypotensive response to hydralazine is less predictable than that seen with other parenteral agents.

Dosing (Adult): Initial (Acute hypertension): 10 mg slow IV bolus (maximum dose being 20 mg) every 4 to 6 hours as needed. May increase to 40 mg/dose (generally speaking - do not exceed 20mg/dose). Change to oral therapy as soon as possible. The fall in blood pressure begins within 10 to 30 minutes and lasts 2 to 4 hours. May also be given IM.

Supplied: Injection (soln): 20 mg/ml (1 ml vial). Tablet: 10 mg, 25 mg, 50 mg, 100 mg.

Labetalol - Trandate ®  top of page

Combined beta-adrenergic (B1 and B2) and alpha-adrenergic blocker. Its rapid onset of action (~ 5 minutes) makes it the only beta-blocker that is useful in the treatment of hypertensive emergencies. Safe in patients with active coronary disease, since it does not increase the heart rate. Labetalol should generally be avoided in patients with asthma, COPD, CHF, bradycardia, or greater than first-degree heart block. Causes marked orthostatic effects.

Dosing (Adult): can be given as an IV bolus or infusion. The bolus dose is 20 mg initially (over 2 min), followed by 20 to 80 mg every 10 minutes to a total dose of 300 mg. The infusion rate is 0.5 to 2 mg/min. Onset/duration: 5-10 min/2-6 hr. Peak effect in 30 minutes.

Hypertension (Oral): Initial: 100 mg twice daily - may increase as needed every 2-3 days by 100 mg until desired response is obtained. Usual dose: 200-400 mg twice daily - not to exceed 2.4 grams/day.

Supplied: Injection (soln): 5 mg/ml: (4 ml, 20 ml, 40 ml). Tablet: 100 mg, 200 mg, 300 mg.

Nicardipine - Cardene ®  top of page

Dihydropyridine calcium channel blocker. Advantages: Does not depress LV function; does not adversely increase ICP (acceptable choice in stroke patients). Major limitation: longer half-life, which precludes rapid titration. Contraindicated in heart block, recent AMI, and renal failure.

Dosing (Adults)
(Acute hypertension) - The initial dose is 5 mg/hour and can be increased to a maximum of 15 mg/hour. Effects seen within 15 minutes. Initial dose of 5 mg/hr can be increased by 2.5 mg/hour every 15 minutes to the previously listed maximum of 15 mg/hour. Consider reduction to 3 mg/hour after response is achieved. Monitor and titrate to lowest dose necessary to maintain stable blood pressure.

Preparation: Dilute to 0.1 mg/ml (25 mg in D5W 250 ml).
Substitution IV to oral therapy (approximate):
0.5 mg/hr IV = ~ 20mg po q8h.
1.2 mg/hr IV = ~ 30mg po q8h.
2.2 mg/hr IV = ~ 40mg po q8h.

(Other indications):
Angina: Immediate release capsule: 20 mg orally 3 times daily. Usual range: 60-120 mg/day. Increase dose at 3 day intervals.
Hypertension: Immediate release capsule: Initial: 20 mg orally 3 times daily. Usual: 20-40 mg 3 times daily (allow 3 days between dose increases). Sustained release capsule: Initial: 30 mg orally twice daily - titrate up to 60 mg twice daily.
Note: The total daily dose of immediate-release product may not automatically be equivalent to the daily sustained-release dose - use caution in converting.

Supplied: Injection (soln): 2.5 mg/ml (10 ml). Capsule (IR): 20 mg, 30 mg. Capsule (SR): 30 mg, 45 mg, 60 mg

Nitroglycerin  top of page

Primarily a venous dilator (lesser degree - arteriolar dilator). It may be most useful in patients with symptomatic coronary disease and in those with hypertension following coronary bypass. Drug of choice for hypertensive emergencies with coronary ischemia. It should not be used with hypertensive encephalopathy because it increases ICP. Tolerance may occur within 24-48 hours. Nitrate-free interval (10-12 hours/day) is recommended to avoid tolerance development.

Dosing (Adults):  (IV): Initial dose: 5 mcg/min IV infusion. Increase by 5 mcg/minute every 3-5 minutes to 20 mcg/minute. If no response at 20 mcg/minute increase by 10 mcg/minute every 3-5 minutes, up to a maximum of 200 mcg/minute.
Onset: 2 to 5 minutes. Duration: 5 to 10 minutes.


Angina/coronary artery disease:
Oral: 2.5mg to 9 mg bid - qid (up to 26 mg qid). Topical ointment: Apply 0.5" to 2" every 6 hours with a nitrate free interval (10-12hrs). Patch (transdermal): 0.2-0.4 mg/hour initially and titrate to doses of 0.4-0.8 mg/hour. Remove patch to provide nitrate free interval (10-12hrs). Sublingual: 0.2-0.6 mg every 5 minutes for maximum of 3 doses in 15 minutes.

Supplied: Capsule (ER): 2.5 mg, 6.5 mg, 9 mg. Injection (Soln): 5 mg/ml (5 ml, 10 ml). Ointment: 2% (1 g, 30 g, 60 g). Sublingual tablet: 0.3 mg, 0.4 mg, 0.6 mg. Patch (Transdermal ): 0.1 mg/hour; 0.2 mg/hour; 0.4 mg/hour; 0.6 mg/hour.

Sodium nitroprusside - Nipride ®  top of page

Arteriolar and venous dilator. Considered to be the most effective parenteral drug for most hypertensive emergencies (except myocardial ischemia or renal impairment). It dilates both arteries and veins, and it reduces afterload and preload. Onset: within seconds. Duration: 2-3 minutes. Constant monitoring of the blood pressure is required.
Alternatives to nitroprusside include intravenous labetalol, nicardipine, and fenoldopam. Hypotension is uncommon with these drugs and cyanide toxicity is not an issue.

Dosing (Adults)Initial: 0.3-0.5 mcg/kg/minute. Increase in increments of 0.5 mcg/kg/minute -- titrating to the desired hemodynamic effect or the appearance of headache or nausea. Usual dose: 3 mcg/kg/minute (rarely need >4 mcg/kg/minute). Maximum: 10 mcg/kg/minute.
 
When treatment is prolonged (>24 to 48 hours) or when renal insufficiency is present, the risk of cyanide and thiocyanate toxicity is increased. Doses > 2 mcg/kg/min exceed the capacity of the body to detoxify cyanide. Maximum doses of 10 mcg/kg/min should never be given for more than 10 minutes. An infusion of sodium thiosulfate can be used in affected patients to provide a sulfur donor to detoxify cyanide into thiocyanate.

Supplied: Injection (Soln): 25 mg/ml - 2 ml (vial).

Reference(s)

National Institutes of Health, U.S. National Library of Medicine, DailyMed Database.
Provides access to the latest drug monographs submitted to the Food and Drug Administration (FDA). Please review the latest applicable package insert for additional information and possible updates.  A local search option of this data can be found here.

Disclaimer

Listed dosages are for - Adult patients ONLY. PLEASE READ THE DISCLAIMER CAREFULLY BEFORE ACCESSING OR USING THIS SITE. BY ACCESSING OR USING THIS SITE, YOU AGREE TO BE BOUND BY THE TERMS AND CONDITIONS SET FORTH IN THE DISCLAIMER. GlobalRPH does not directly or indirectly practice medicine or provide medical services and therefore assumes no liability whatsoever of any kind for the information and data accessed through the Service or for any diagnosis or treatment made in reliance thereon.

David F. McAuley, Pharm.D., R.Ph.  GlobalRPh Inc.
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